Efficient continuous synthesis of 2-[3-(trifluoromethyl)phenyl]malonic acid,a key intermediate of Triflumezopyrim,coupling with esterification-condensation-hydrolysis  

作　　者：Yuexiang Liu Xiangqiao Yang Tong Lin Guantian Yang Xiaoyong Xu Bubing Zeng Zhong Li Weiping Zhu Xuhong Qian 

机构地区：[1]Shanghai Key Laboratory of Chemical Biology,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China [2]Shanghai Frontiers Science Center of Optogenetic Techniques for Cexll Metabolism,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China [3]State Key Laboratory of Bioreactor Engineering,East China University of Science and Technology,Shanghai 200237,China [4]Engineering Research Center of Pharmaceutical Process Chemistry,Ministry of Education,School of Pharmacy,East China University of Science and Technology,Shanghai 200237,China [5]Shanghai Key Laboratory of Green Chemistry and Chemical Processes,Department of Chemistry,School of Chemistry and Molecular Engineering,East China Normal University,Shanghai 200241,China

出　　处：《Chinese Chemical Letters》2025年第1期234-238,共5页中国化学快报(英文版)

基　　金：the National Key Research and Development Program of China(Nos.2023YFD1700303,2022YFD17800);National Natural Science Foundation of China(Nos.21878088,21476077)for financial support。

摘　　要：Triflumezopyrim(TFM)is a novel mesoionic pyrido[1,2-α]pyrimidinones insecticide,which acts on nicotinic acetylcholine receptors(n ACh Rs)and has no cross-resistance with other insecticides.Herein,we firstly developed a new continuous flow approach to synthesis 2-[3-(trifluoromethyl)phenyl]malonic acid,a key intermate of TFM,coupling with esterification,condensation,and hydrolysis.All three-step reactions were optimized and transformed into a continuous synthesis mode by three micro reaction units.Compared with the batch mode,the total reaction time and overall separation yield were improved from more than 12 h and 60%to 18 min and 73.38%,respectively.The solvent consumption and waste emission were significantly reduced,which also provides an eco-friendly and efficient potential tool for the development and production of mesoionic pyrido[1,2-α]pyrimidinones insecticide.

关 键 词：Triflumezopyrim(TFM) 2-[3-(Trifluoromethyl)phenyl]malonic acid Continuous flow synthesis MICRO-REACTOR 

分 类 号：O62[理学—有机化学]